Biological Activity
C188-9 (TTI 101) is a potent STAT3 inhibitor, binds STAT3 with high affinity, Kd=4.7±0.4 nM. It is well tolerated in mice, has good oral bioavailability, and is mainly enriched in tumor tissues.
in vitro
C188-9 is a small molecule inhibitor of STAT3, targeting the phosphotyrosine peptide binding site in the SH2 region of STAT3 with a Ki value of 136 nM. It does not inhibit upstream Jak or Src kinases.
in vivo
C188-9 inhibited tumor growth in mice bearing UM-SCC-17B xenografts after administration of C188-9. C188-9 was well tolerated in mice, had good oral bioavailability, and was concentrated in tumor tissue after administration.
target
| Target | Value |
STAT3
(Cell-free) | 4.7 nM(Kd) |
